hydroxyzine Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
diphenylmethyl piperazine derivatives 1400 68-88-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • hydroxyzine pamoate
  • hydroxizine
  • hydroxyzin
  • hydroxyzyne
  • tranquizine
  • hydroxyzine
  • hydroxyzine hydrochloride
  • hydroxyzine dihydrochloride
  • hydroxyzine HCl
A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.
  • Molecular weight: 374.91
  • Formula: C21H27ClN2O2
  • CLOGP: 4
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 1
  • TPSA: 35.94
  • ALOGS: -3.61
  • ROTB: 8

Drug dosage:

DoseUnitRoute
75 mg O
75 mg P

Approvals:

DateAgencyCompanyOrphan
April 12, 1956 FDA PFIZER

FDA Adverse Event Reporting System

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Completed suicide 2828.82 44.59 646 1870 30468 3352875
Toxicity to various agents 1636.26 44.59 457 2059 46597 3336746
Cardiac arrest 757.73 44.59 225 2291 27094 3356249
Poisoning 748.83 44.59 160 2356 4952 3378391
Respiratory arrest 696.00 44.59 175 2341 11193 3372150
Drug abuse 695.58 44.59 193 2323 18137 3365206
Drug hypersensitivity 580.74 44.59 196 2320 35484 3347859
Cardio-respiratory arrest 491.29 44.59 142 2374 15298 3368045
Overdose 410.97 44.59 150 2366 33828 3349515
Death 367.76 44.59 219 2297 152105 3231238
Intentional overdose 341.05 44.59 107 2409 15118 3368225
Exposure via ingestion 276.87 44.59 57 2459 1436 3381907
Intentional product misuse 237.82 44.59 78 2438 12623 3370720
Chronic spontaneous urticaria 157.09 44.59 23 2493 60 3383283
Electrocardiogram QT prolonged 145.91 44.59 52 2464 10743 3372600
Suicide attempt 133.35 44.59 54 2462 15793 3367550
Hypotension 122.40 44.59 73 2443 49441 3333902
Somnolence 113.59 44.59 60 2456 32144 3351199
Urticaria 111.27 44.59 57 2459 28670 3354673
Drug ineffective 99.22 44.59 90 2426 116000 3267343
Angioedema 98.55 44.59 43 2473 15092 3368251
Pruritus 97.68 44.59 62 2454 46771 3336572
Torsade de pointes 96.38 44.59 28 2488 3001 3380342
Shock 95.86 44.59 34 2482 6903 3376440
Coma 92.72 44.59 39 2477 12513 3370830
Agitation 75.91 44.59 39 2477 19667 3363676
Bradycardia 73.03 44.59 36 2480 16633 3366710
Condition aggravated 72.05 44.59 48 2468 39185 3344158
Mental status changes 69.84 44.59 30 2486 10117 3373226
Unresponsive to stimuli 69.71 44.59 28 2488 7980 3375363
Acute generalised exanthematous pustulosis 69.41 44.59 20 2496 2079 3381264
Tachycardia 66.94 44.59 38 2478 23333 3360010
Drug interaction 66.65 44.59 49 2467 46763 3336580
Cardiomegaly 66.57 44.59 23 2493 4315 3379028
Insomnia 66.09 44.59 44 2472 35854 3347489
Confusional state 63.81 44.59 44 2472 37954 3345389
Poisoning deliberate 63.25 44.59 16 2500 1015 3382328
Electrocardiogram QRS complex prolonged 59.02 44.59 16 2500 1330 3382013
Pulmonary congestion 57.98 44.59 19 2497 3031 3380312
Drug screen positive 57.69 44.59 17 2499 1911 3381432
Acute respiratory distress syndrome 56.14 44.59 22 2494 5872 3377471
Foetal exposure during pregnancy 54.77 44.59 29 2487 15522 3367821
Nodular rash 52.28 44.59 9 2507 81 3383262
Ventricular fibrillation 51.45 44.59 19 2497 4314 3379029
Aspiration 50.69 44.59 17 2499 2911 3380432
Loss of consciousness 50.56 44.59 34 2482 28113 3355230
Anticholinergic syndrome 50.56 44.59 11 2505 360 3382983
Hepatic steatosis 49.10 44.59 19 2497 4901 3378442
Seizure 48.00 44.59 38 2478 40362 3342981
Depressed level of consciousness 47.92 44.59 24 2492 11441 3371902
Lactic acidosis 47.75 44.59 21 2495 7479 3375864
Tonsillar hypertrophy 46.67 44.59 10 2506 304 3383039
Respiratory depression 46.21 44.59 17 2499 3817 3379526
Accidental overdose 45.54 44.59 20 2496 7098 3376245
Accidental death 44.62 44.59 11 2505 627 3382716

Pharmacologic Action:

SourceCodeDescription
ATC N05BB01 NERVOUS SYSTEM
PSYCHOLEPTICS
ANXIOLYTICS
Diphenylmethane derivatives
ATC N05BB51 NERVOUS SYSTEM
PSYCHOLEPTICS
ANXIOLYTICS
Diphenylmethane derivatives
MeSH PA D000982 Antipruritics
MeSH PA D003879 Dermatologic Agents
MeSH PA D018494 Histamine Agents
MeSH PA D006633 Histamine Antagonists
MeSH PA D006634 Histamine H1 Antagonists
MeSH PA D018377 Neurotransmitter Agents
CHEBI has role CHEBI:37955 H1-receptor antagonist
CHEBI has role CHEBI:35474 anxiolytic drug
CHEBI has role CHEBI:50177 dermatologic drug
CHEBI has role CHEBI:59683 antipruritic drug
FDA EPC N0000175750 Antihistamine
FDA MoA N0000000207 Histamine Receptor Antagonists

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Dermatographic urticaria indication 7632005 DOID:743
Atopic dermatitis indication 24079001 DOID:3310
Allergic rhinitis indication 61582004
Nasal discharge indication 64531003
Urticaria indication 126485001
Itching of skin indication 418363000
Allergic conjunctivitis indication 473460002 DOID:11204
Severe Pruritus off-label use
Tachyarrhythmia contraindication 6285003
Alcoholism contraindication 7200002
Peptic ulcer contraindication 13200003 DOID:750
Pulmonary edema contraindication 19242006 DOID:11396
Myocardial infarction contraindication 22298006 DOID:5844
Shock contraindication 27942005
Hyperthyroidism contraindication 34486009 DOID:7998
Acute hepatitis contraindication 37871000
Hypertensive disorder contraindication 38341003 DOID:10763
Hypothyroidism contraindication 40930008 DOID:1459
Third trimester pregnancy contraindication 41587001
Conduction disorder of the heart contraindication 44808001
Chronic heart failure contraindication 48447003
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Multiple organ failure contraindication 57653000
Psychotic disorder contraindication 69322001
Diabetes mellitus contraindication 73211009 DOID:9351
Chronic idiopathic constipation contraindication 82934008
Cor pulmonale contraindication 83291003 DOID:8515
Open-angle glaucoma contraindication 84494001 DOID:1067
Seizure disorder contraindication 128613002 DOID:1826
Cystic fibrosis contraindication 190905008 DOID:1485
Angina pectoris contraindication 194828000
Disease of liver contraindication 235856003 DOID:409
Bladder outflow obstruction contraindication 236645006
Sepsis syndrome contraindication 238150007
Benign prostatic hyperplasia contraindication 266569009 DOID:2883
Retention of urine contraindication 267064002
Continuous fever contraindication 271751000
Smoking cessation assistance contraindication 384742004
Angle-closure glaucoma contraindication 392291006 DOID:13550
Chronic myocardial ischemia contraindication 413844008 DOID:3393
Disorder of coronary artery contraindication 414024009
Myocardial ischemia contraindication 414795007 DOID:3393
Smokes tobacco daily contraindication 449868002
Severe Hypoxemia contraindication
Theophylline Toxicity contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.53 Basic
pKa2 3.53 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Histamine H1 receptor GPCR ANTAGONIST Ki 8.70 WOMBAT-PK CHEMBL
Cytochrome P450 2D6 Enzyme Ki 5.41 WOMBAT-PK
Envelope glycoprotein gp160 Unclassified IC50 5.20 CHEMBL

External reference:

IDSource
DB00557 DRUGBANK_ID
4019782 VUID
N0000147873 NUI
C0020404 UMLSCUI
7199 IUPHAR_LIGAND_ID
D00672 KEGG_DRUG
30S50YM8OG UNII
599 INN_ID
2192-20-3 SECONDARY_CAS_RN
CHEMBL896 ChEMBL_ID
5553 RXNORM
372856003 SNOMEDCT_US
80165005 SNOMEDCT_US
4857 MMSL
d00907 MMSL
4019782 VANDF
N0000007299 NDFRT
N0000147873 NDFRT
001451 NDDF
3658 PUBCHEM_CID
CHEMBL1200467 ChEMBL_ID
CHEMBL1201007 ChEMBL_ID
D006919 MESH_DESCRIPTOR_UI
CHEBI:5818 CHEBI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-5060 TABLET, FILM COATED 10 mg ORAL ANDA 12 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-5061 TABLET, FILM COATED 25 mg ORAL ANDA 12 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-5062 TABLET, FILM COATED 50 mg ORAL ANDA 12 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0121-4822 SYRUP 10 mg ORAL ANDA 12 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0179-0072 TABLET, FILM COATED 25 mg ORAL ANDA 12 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0179-0075 TABLET, FILM COATED 10 mg ORAL ANDA 12 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-2586 TABLET, FILM COATED 10 mg ORAL ANDA 11 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-2587 TABLET, FILM COATED 25 mg ORAL ANDA 11 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0378-2588 TABLET, FILM COATED 50 mg ORAL ANDA 11 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0440-1617 TABLET, FILM COATED 25 mg ORAL ANDA 10 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0517-4201 INJECTION, SOLUTION 25 mg INTRAMUSCULAR ANDA 11 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0517-5601 INJECTION, SOLUTION 50 mg INTRAMUSCULAR ANDA 11 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0517-5602 INJECTION, SOLUTION 50 mg INTRAMUSCULAR ANDA 11 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0517-5610 INJECTION, SOLUTION 50 mg INTRAMUSCULAR ANDA 11 sections
Hydroxyzine HUMAN PRESCRIPTION DRUG LABEL 1 0615-1525 TABLET, FILM COATED 10 mg ORAL ANDA 13 sections
Hydroxyzine HUMAN PRESCRIPTION DRUG LABEL 1 0615-1526 TABLET, FILM COATED 25 mg ORAL ANDA 13 sections
Hydroxyzine HUMAN PRESCRIPTION DRUG LABEL 1 0615-1527 TABLET, FILM COATED 50 mg ORAL ANDA 13 sections
Hydroxyzine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-8037 TABLET 25 mg ORAL ANDA 11 sections
Hydroxyzine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-8082 TABLET 25 mg ORAL ANDA 11 sections
Hydroxyzine HUMAN PRESCRIPTION DRUG LABEL 1 0904-0357 TABLET, FILM COATED 10 mg ORAL ANDA 12 sections
Hydroxyzine HUMAN PRESCRIPTION DRUG LABEL 1 0904-0358 TABLET, FILM COATED 25 mg ORAL ANDA 12 sections
Hydroxyzine HUMAN PRESCRIPTION DRUG LABEL 1 0904-0359 TABLET, FILM COATED 50 mg ORAL ANDA 12 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0904-6617 TABLET, FILM COATED 25 mg ORAL ANDA 11 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0904-6618 TABLET, FILM COATED 50 mg ORAL ANDA 11 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 10544-017 TABLET, FILM COATED 25 mg ORAL ANDA 10 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 10544-043 TABLET, FILM COATED 10 mg ORAL ANDA 10 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 10544-091 TABLET, FILM COATED 10 mg ORAL ANDA 10 sections
Hydroxyzine HUMAN PRESCRIPTION DRUG LABEL 1 10544-209 TABLET, FILM COATED 10 mg ORAL ANDA 12 sections
Hydroxyzine HUMAN PRESCRIPTION DRUG LABEL 1 10544-210 TABLET, FILM COATED 25 mg ORAL ANDA 12 sections
Hydroxyzine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 10544-226 TABLET, FILM COATED 25 mg ORAL ANDA 11 sections